EP2927232A4 - Heteroaryl alkyne compound and application thereof - Google Patents

Heteroaryl alkyne compound and application thereof

Info

Publication number
EP2927232A4
EP2927232A4 EP13859519.4A EP13859519A EP2927232A4 EP 2927232 A4 EP2927232 A4 EP 2927232A4 EP 13859519 A EP13859519 A EP 13859519A EP 2927232 A4 EP2927232 A4 EP 2927232A4
Authority
EP
European Patent Office
Prior art keywords
application
alkyne compound
heteroaryl
heteroaryl alkyne
compound
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP13859519.4A
Other languages
German (de)
French (fr)
Other versions
EP2927232A1 (en
Inventor
Yong Wang
Liwen Zhao
Di Zhang
Feng Wu
Sheng Bi
Yiping Gao
Hongbin Chen
Hongyan Chen
Cang Zhang
Yang Nan
Yang Liu
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Nanjing Sanhome Pharmaceutical Co Ltd
Original Assignee
Nanjing Sanhome Pharmaceutical Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Nanjing Sanhome Pharmaceutical Co Ltd filed Critical Nanjing Sanhome Pharmaceutical Co Ltd
Publication of EP2927232A1 publication Critical patent/EP2927232A1/en
Publication of EP2927232A4 publication Critical patent/EP2927232A4/en
Withdrawn legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4196—1,2,4-Triazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/64—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with substituted hydrocarbon radicals attached to ring carbon atoms, e.g. histidine
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/91—Nitro radicals
    • C07D233/92—Nitro radicals attached in position 4 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
EP13859519.4A 2012-11-28 2013-11-27 Heteroaryl alkyne compound and application thereof Withdrawn EP2927232A4 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN201210493364.9A CN103848829B (en) 2012-11-28 2012-11-28 Heteroaryl alkyne compounds and application thereof
PCT/CN2013/087944 WO2014082578A1 (en) 2012-11-28 2013-11-27 Heteroaryl alkyne compound and application thereof

Publications (2)

Publication Number Publication Date
EP2927232A1 EP2927232A1 (en) 2015-10-07
EP2927232A4 true EP2927232A4 (en) 2016-08-10

Family

ID=50827191

Family Applications (1)

Application Number Title Priority Date Filing Date
EP13859519.4A Withdrawn EP2927232A4 (en) 2012-11-28 2013-11-27 Heteroaryl alkyne compound and application thereof

Country Status (9)

Country Link
US (1) US9255107B2 (en)
EP (1) EP2927232A4 (en)
JP (1) JP2016500118A (en)
KR (1) KR20150074186A (en)
CN (2) CN103848829B (en)
AU (1) AU2013351622A1 (en)
CA (1) CA2891851A1 (en)
HK (1) HK1208438A1 (en)
WO (1) WO2014082578A1 (en)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN104341416B (en) * 2013-07-31 2017-03-29 南京圣和药业股份有限公司 Protein tyrosine kinase inhibitor and its application
WO2015058661A1 (en) * 2013-10-23 2015-04-30 南京圣和药业股份有限公司 Bcr-abl kinase inhibitor and application thereof
GB2522226A (en) * 2014-01-17 2015-07-22 Agency Science Tech & Res Heteroaryl alkyne derivatives and uses thereof
CN105153026B (en) * 2015-08-21 2018-02-02 江西科技师范大学 Sorafenib derivative of the amide structure containing biaryl and its preparation method and application
CN106632146A (en) * 2015-10-28 2017-05-10 南京圣和药业股份有限公司 A diynyl compound and a synthetic method thereof
WO2017152126A1 (en) 2016-03-03 2017-09-08 Cornell University Small molecule ire1-alpha inhibitors
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
CN107226809A (en) * 2016-03-23 2017-10-03 浙江大德药业集团有限公司 Tyrosine kinase inhibitor
RU2652992C2 (en) 2016-04-18 2018-05-04 Общество С Ограниченной Ответственностью "Фьюжн Фарма" Novel crystalline salt form 3-(1,2,4-triazolo[4,3-a]pyridin-3-ylethynyl)-4-methyl-n-(4-((4-methylpiperazin-1-yl)methyl)-3-trifluoromethylphenyl) benzamide for medical application
CN108473476B (en) * 2016-10-13 2021-02-19 深圳市塔吉瑞生物医药有限公司 Alkynyl heterocyclic compounds for inhibiting protein kinase activity
WO2018089736A1 (en) * 2016-11-10 2018-05-17 Dana-Farber Cancer Institute, Inc. Degradation of protein kinases by conjugation of protein kinase inhibitors with e3 ligase ligand and methods of use
WO2018161033A1 (en) * 2017-03-02 2018-09-07 Wright, Adrian Small molecule ire1-alpha inhibitors
CN116444525A (en) * 2023-03-27 2023-07-18 成都苑东生物制药股份有限公司 Preparation method of ponatinib hydrochloride A crystal form

Citations (2)

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WO2007133560A2 (en) * 2006-05-08 2007-11-22 Ariad Pharmaceuticals, Inc. Acetylenic heteroaryl compounds
WO2012000304A1 (en) * 2010-07-01 2012-01-05 中国科学院广州生物医药与健康研究院 Heterocyclic alkynyl benzene compounds and medical compositions and uses thereof

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US7776869B2 (en) * 2004-10-18 2010-08-17 Amgen Inc. Heteroaryl-substituted alkyne compounds and method of use
JP5200939B2 (en) 2005-12-23 2013-06-05 アリアド・ファーマシューティカルズ・インコーポレイテッド Bicyclic heteroaryl compounds
CN101389338B (en) * 2005-12-23 2013-06-26 阿里亚德医药股份有限公司 Bicyclic heteroaryl compounds
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AU2007249926B8 (en) 2006-05-08 2013-11-07 Ariad Pharmaceuticals, Inc. Monocyclic heteroaryl compounds
EP2070929A1 (en) * 2007-12-11 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Alkynylaryl compounds and salts thereof, pharmaceutical compositions comprising same, methods of preparing same and uses of same
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WO2007133560A2 (en) * 2006-05-08 2007-11-22 Ariad Pharmaceuticals, Inc. Acetylenic heteroaryl compounds
WO2012000304A1 (en) * 2010-07-01 2012-01-05 中国科学院广州生物医药与健康研究院 Heterocyclic alkynyl benzene compounds and medical compositions and uses thereof
EP2594567A1 (en) * 2010-07-01 2013-05-22 Guangzhou Institute Of Biomedicine And Health, Chinese Academy Of Sciences Heterocyclic alkynyl benzene compounds and medical compositions and uses thereof

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Title
BIMBISAR DESAI ET AL: "Rapid Discovery of a Novel Series of Abl Kinase Inhibitors by Application of an Integrated Microfluidic Synthesis and Screening Platform", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 7, 11 April 2013 (2013-04-11), US, pages 3033 - 3047, XP055253098, ISSN: 0022-2623, DOI: 10.1021/jm400099d *
DENG XIANMING ET AL: "Broad spectrum alkynyl inhibitors of T315I Bcr-Abl", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 20, no. 14, 19 May 2010 (2010-05-19), pages 4196 - 4200, XP029121028, ISSN: 0960-894X, DOI: 10.1016/J.BMCL.2010.05.043 *
HUANG WEI-SHENG ET AL: "Discovery of 3-[2-(Imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{ 4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a Potent, Orally Active Pan-Inhibitor of Breakpoint Cluster Region-Abelson (BCR-ABL) Kinase Including the T315I Gatekeeper Mutant", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 53, no. 12, 24 June 2010 (2010-06-24), pages 4701 - 4719, XP002615777, ISSN: 0022-2623, [retrieved on 20100601], DOI: 10.1021/JM100395Q *
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XIAOMEI REN ET AL: "Identification of GZD824 as an Orally Bioavailable Inhibitor That Targets Phosphorylated and Nonphosphorylated Breakpoint Cluster Region-Abelson (Bcr-Abl) Kinase and Overcomes Clinically Acquired Mutation-Induced Resistance against Imatinib", JOURNAL OF MEDICINAL CHEMISTRY, vol. 56, no. 3, 14 February 2013 (2013-02-14), pages 879 - 894, XP055099026, ISSN: 0022-2623, DOI: 10.1021/jm301581y *

Also Published As

Publication number Publication date
US20150299202A1 (en) 2015-10-22
CN104797581A (en) 2015-07-22
CN103848829A (en) 2014-06-11
JP2016500118A (en) 2016-01-07
WO2014082578A1 (en) 2014-06-05
KR20150074186A (en) 2015-07-01
AU2013351622A1 (en) 2015-06-04
US9255107B2 (en) 2016-02-09
CN103848829B (en) 2017-04-12
HK1208438A1 (en) 2016-03-04
CA2891851A1 (en) 2014-06-05
CN104797581B (en) 2017-02-15
EP2927232A1 (en) 2015-10-07

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